scholarly journals Design, Synthesis and Antibacterial Activity of some 3,6-Dimethlyquinoxaline-2-Hydrazone Derivatives

Author(s):  
F. O. Taiwo ◽  
C. A. Obafemi ◽  
D. A. Akinpelu ◽  
T. O. Iyiola

Aims: This aims of this study was to continue the effort to synthesis new quinoxaline-based heterocycles and study its antibacterial properties. Objective: This study was designed to reacts 3,6-dimethylquinoxaline-2-hydrazine with some substituted aromatic ketones and study their antibacterial properties on some locally and clinically isolated bacterial strains. Materials and Methods: Five 3,6-dimethylquinoxaline-2-hydrazone derivatives were synthesized from the reactions of 3,6-dimethylquinoxaline-2-hydrazine with various substituted aromatic ketones. The products were then tested for their potential antibacterial properties. Results: All the synthesized compounds were found to be active against all the bacterial strains investigated in this study. It was observed that the zones of inhibition observed for the synthesized compounds against the test organisms ranged between 15 mm and 38 mm. The MIC observed for the synthesized compounds ranged between 0.0313mg/mL and 0.125 mg/mL, while that of the standard antibiotic, streptomycin, varied between 0.0313 mg/mL and 0.500 mg/mL and those observed for tetracycline falls between 0.0313 mg/mL and 0.500 mg/mL. The minimum bactericidal concentrations exhibited by the synthesized compounds ranged between 0.0625 mg/mL and 0.250 mg/mL Discussion and conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects against all the bacterial strains, which is an indication that such synthetic compounds possessed broad spectrum activities and such compounds could be useful in formulation of antibacterial compounds which could be used to mitigates infections caused by pathogens that are now developing resistance against the available antibiotics.

Author(s):  
F. O. Taiwo ◽  
C.A. Obafemi ◽  
D.A. Akinpelu

Aims: This aims of this study was to synthesis new quinoxaline-based heterocycles and study its antibacterial properties. Objective: This study was designed to synthesis some 3-methyl-6-nitroquinoxaline-2-one with hydrazine moiety, characterize the synthesized compounds, and study their antibacterial properties on some bacterial strains. Materials and Methods: Six 3-methylquinoxaline-2-hydrazone derivatives were synthesized by reacting 2-hydrazinyl-3-methyl-6-nitroquinoxaline with various substituted acetophenones. The hydrazones were screened for their potential antibacterial properties. Results: All the test compounds were found to possessed promising antibacterial properties against a panel of bacterial strains screened for this study. The MIC values exhibited by these compounds ranged between 0.0313 and 0.250 mg/mL. The lowest MBC of the compounds against the test organism was 0.0625 mg/mL while the highest MBC was 0.250 mg/mL. Discussion and Conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects against all the bacterial strains, which is an indication that such synthetic compounds possessed broad spectrum activities and such compounds could be useful in formulation of antibacterial compounds which could be used to mitigates infections caused by pathogens that are now developing resistance against the available antibiotics.


2016 ◽  
Vol 1 (1-2) ◽  
pp. 05-09 ◽  
Author(s):  
Samuel L. Oputah ◽  
Kolawole O. Ajanaku ◽  
Raphael C. Mordi ◽  
Joseph A. O. Olugbuyiro ◽  
Shade J. Olorunshola ◽  
...  

Phytochemical and antibacterial properties of ethanolic extract of the seeds of African Star Apple (Chrysophyllum albidum) were investigated. The phytochemical result revealed the presence of saponins, carbohydrates, flavonoids, quinones, cardiac glycosides, fatty acids and terpenoids. The antibacterial activity was studied using agar well diffusion method at different concentrations against six pathogenic bacterial strains, three Gram-positive (Staphylococcus aureus, Micrococcus varians and Bacillus cereus) and three Gram-negative (Escherichia coli, Pseudomonas aeruginosa and Proteus vulgaris). Significant inhibitory activities were exhibited by the ethanolic seed extracts for all test organisms except Bacillus cereus. Zone of inhibition of the crude ethanolic extract was correlated with that of a standard antibiotic Gentamicin, for antibacterial activity. The results indicated a notable inhibition of the bacterial growth.


Author(s):  
Festus O. Taiwo ◽  
Craig A. Obafemi ◽  
David A. Akinpelu A. Akinpelu

Aims: This studies aims at the synthesis of new heterocyclic systems and study its biological and pharmacological properties. Objective: This study was designed to synthesized some quinoxaline-2,3-dione with sulfonamide moiety, characterize the synthesized compounds, and study the antimicrobial properties of the synthesized compounds on some bacterial strains. Materials and Methods: Six quinoxaline-6-sulfonohydrazone derivatives were synthesized by reacting quinoxaline-6-sulfonohydrazine with some substituted benzaldehydes and ketones. The compounds were tested for their potential antibacterial properties. Results: All the test compounds possessed promising antibacterial property against a panel of bacterial strains used for this study. The MIC values exhibited by these compounds ranged between 0.0313 and 0.250 mg/mL. Among the compounds tested, compound 2 showed appreciable antibacterial activity. Discussion and Conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects towards all the bacterial strains, particularly, compound 2 This is an indication that such compounds possessing broad spectrum activities will be useful in formulating antimicrobial compounds which could be used to treat infections caused by pathogens that are now developing resistance against the available antibiotics.


Materials ◽  
2021 ◽  
Vol 14 (14) ◽  
pp. 3854
Author(s):  
Joanna Czechowska ◽  
Ewelina Cichoń ◽  
Anna Belcarz ◽  
Anna Ślósarczyk ◽  
Aneta Zima

Bioactive, chemically bonded bone substitutes with antibacterial properties are highly recommended for medical applications. In this study, biomicroconcretes, composed of silicon modified (Si-αTCP) or non-modified α-tricalcium phosphate (αTCP), as well as hybrid hydroxyapatite/chitosan granules non-modified and modified with gold nanoparticles (AuNPs), were designed. The developed biomicroconcretes were supposed to combine the dual functions of antibacterial activity and bone defect repair. The chemical and phase composition, microstructure, setting times, mechanical strength, and in vitro bioactive potential of the composites were examined. Furthermore, on the basis of the American Association of Textile Chemists and Colorists test (AATCC 100), adapted for chemically bonded materials, the antibacterial activity of the biomicroconcretes against S. epidermidis, E. coli, and S. aureus was evaluated. All biomicroconcretes were surgically handy and revealed good adhesion between the hybrid granules and calcium phosphate-based matrix. Furthermore, they possessed acceptable setting times and mechanical properties. It has been stated that materials containing AuNPs set faster and possess a slightly higher compressive strength (3.4 ± 0.7 MPa). The modification of αTCP with silicon led to a favorable decrease of the final setting time to 10 min. Furthermore, it has been shown that materials modified with AuNPs and silicon possessed an enhanced bioactivity. The antibacterial properties of all of the developed biomicroconcretes against the tested bacterial strains due to the presence of both chitosan and Au were confirmed. The material modified simultaneously with AuNPs and silicon seems to be the most promising candidate for further biological studies.


Chemistry ◽  
2021 ◽  
Vol 3 (3) ◽  
pp. 783-799
Author(s):  
Maryam Ariannezhad ◽  
Davood Habibi ◽  
Somayyeh Heydari ◽  
Vahideh Khorramabadi

A new magnetic supported manganese-based coordination complex (Fe3O4@SiO2@CPTMS@MBOL@ Mn) was prepared in consecutive stages and characterized via various techniques (VSM, SEM, TEM, XRD, FT-IR, EDX, TG-DTA, and ICP). To evaluate its application, it was used for synthesis of divers Indazolophthalazinetriones in a simple procedure via the one-pot three-component condensation reaction of aldehydes, dimedone, and phthalhydrazide in ethanol under reflux conditions. The Mn catalyst can be recycled without any noticeable loss in catalytic activity. Additionally, the antibacterial properties of the nano-catalyst were studied against some bacterial strains.


Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3109 ◽  
Author(s):  
Andres Bernal-Ballen ◽  
Jorge Lopez-Garcia ◽  
Martha-Andrea Merchan-Merchan ◽  
Marian Lehocky

Bio-artificial polymeric systems are a new class of polymeric constituents based on blends of synthetic and natural polymers, designed with the purpose of producing new materials that exhibit enhanced properties with respect to the individual components. In this frame, a combination of polyvinyl alcohol (PVA) and chitosan, blended with a widely used antibiotic, sodium ampicillin, has been developed showing a moderate behavior in terms of antibacterial properties. Thus, aqueous solutions of PVA at 1 wt.% were mixed with acid solutions of chitosan at 1 wt.%, followed by adding ampicillin ranging from 0.3 to 1.0 wt.% related to the total amount of the polymers. The prepared bio-artificial polymeric system was characterized by FTIR, SEM, DSC, contact angle measurements, antibacterial activity against Staphylococcus aureus and Escherichia coli and antibiotic release studies. The statistical significance of the antibacterial activity was determined using a multifactorial analysis of variance with ρ < 0.05 (ANOVA). The characterization techniques did not show alterations in the ampicillin structure and the interactions with polymers were limited to intermolecular forces. Therefore, the antibiotic was efficiently released from the matrix and its antibacterial activity was preserved. The system disclosed moderate antibacterial activity against bacterial strains without adding a high antibiotic concentration. The findings of this study suggest that the system may be effective against healthcare-associated infections, a promising view in the design of novel antimicrobial biomaterials potentially suitable for tissue engineering applications.


2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Agata Cieślik-Bielecka ◽  
Tadeusz Bold ◽  
Grzegorz Ziółkowski ◽  
Marcin Pierchała ◽  
Aleksandra Królikowska ◽  
...  

The aim of the study was to investigate the leukocyte- and platelet-rich plasma (L-PRP) antimicrobial activity. The studied sample comprised 20 healthy males. The L-PRP gel, liquid L-PRP, and thrombin samples were testedin vitrofor their antibacterial properties against selected bacterial strains using the Kirby-Bauer disc diffusion method. Two types of thrombin were used (autologous and bovine). Zones of inhibition produced by L-PRP ranged between 6 and 18 mm in diameter. L-PRP inhibited the growth ofStaphylococcus aureus(MRSA and MSSA strains) and was also active againstEnterococcus faecalisandPseudomonas aeruginosa. There was no activity againstEscherichia coliandKlebsiella pneumoniae. The statistically significant increase of L-PRP antimicrobial effect was noted with the use of major volume of thrombin as an activator. Additionally, in groups where a bovine thrombin mixture was added to L-PRP the zones of inhibition concerning MRSA,Enterococcus faecalis, andPseudomonas aeruginosawere larger than in the groups with autologous thrombin. Based on the conducted studies, it can be determined that L-PRP can evokein vitroantimicrobial effects and might be used to treat selected infections in the clinical field. The major volume of thrombin as an activator increases the strength of the L-PRP antimicrobial effect.


2014 ◽  
Vol 875-877 ◽  
pp. 87-90 ◽  
Author(s):  
Chutimon Satirapipathkul ◽  
Tanakan Chatdum

The film-forming potential of isolate of seed polysaccharide fromCassia fistulawas investigated. Increasing the glycerol concentration in the film increased elongation at break, film solubility and water vapor permeability but decreased tensile strength (TS). The film impregnated with the acetone extract ofAtractylodes lanceawas assessed for inhibition ofEscherichia coliandStaphylococcus aureus. The obtained results showed that the films exhibited antibacterial activity against both bacterial strains. Disc-diffusion assay revealed that the film resulted in a larger inhibition zone around the film onStaphylococcus aureusthan it did onEscherichia coliat the same extract concentrations (0.1 to 0.9 wt %). It can be seen that the film has satisfactory physical and antibacterial properties.


Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2126 ◽  
Author(s):  
Alla V. Lipeeva ◽  
Danila O. Zakharov ◽  
Liubov G. Burova ◽  
Tatyana S. Frolova ◽  
Dmitry S. Baev ◽  
...  

Synthesis of 1,2,3-triazole-substituted coumarins and also 1,2,3-triazolyl or 1,2,3-triazolylalk-1-inyl-linked coumarin-2,3-furocoumarin hybrids was performed by employing the cross-coupling and copper catalyzed azide-alkyne cycloaddition reaction approaches. The synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, Bacillius subtilis, Actinomyces viscosus and Escherichia coli bacterial strains. Coumarin-benzoic acid hybrids 4с, 42с and 3-((4-acetylamino-3-(methoxycarbonyl)phenyl)ethynyl)coumarin (29) showed promising activity against S. aureus strains, and the 1,2,3-triazolyloct-1-inyl linked coumarin-2,3-furocoumarin hybrid 37c was endowed with high selectivity against B. subtilis and E. coli species. The in vitro antibacterial activity of 4с, 29, 37c and 42с can potentially be compared with that of a number of modern antibiotic drugs used in the clinic, suggesting promising prospects for further research. A detailed study of the molecular interactions with the targeted protein MurB was performed using docking simulations and the obtained results are quite promising.


2021 ◽  
pp. e304
Author(s):  
Candy GERGES ◽  
Mohamad HADLA ◽  
Michele ELIALI ◽  
Martine RICHA ◽  
Nour Mammari ◽  
...  

Background: Thousands of people are dying as a result of infections caused by bacteria. Among the main routes of germ transmission are the hands, making hand hygiene very important in preventing the spread of pathogens and bacterial infection. Hand washing with soap and water is considered to be a simple and effective measure. Old soap manufacturers have long had traditional uses in the Lebanese community. Methods: The purpose of this study is to compare the antibacterial activity of oil-based soaps with commercial soap sold in the Lebanese market. Different types of herbal soap and antiseptics have been used in this study. Four bacterial strains were used: Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, Escherichia coli and Enterobacter Spp. The antibacterial activities of these soaps were determined by the diffusion method of disks in agar medium. Results and Discussion: Statistical analysis of zones of inhibition showed that S. epidermidis, P. aeruginosa and Enterobacter Spp. were sensitive only to traditional oil-based soaps, which are Sage, Rose Mary and Cedar. In addition, S. aureus showed sensitivity to soaps comprised of essential oils as well as antibacterial synthetic soap, Dettol and Lifebuoy. On the other hand, E. coli showed resistance to all soaps. Soaps comprised of natural essential oils have shown antibacterial activity superior to so-called “Antibacterial” soaps. Conclusion: Based on this study, we can say that the use of soaps with essential oils might be the best option due to their organic origin as well as their antibacterial proved activities.


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